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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Setipiprant (ACT-129968 and KYTH-105) is a novel, potent, orally bioavailable and selective CRTH2 antagonist. It has been demonstrated to be more specific for DP2 (prostaglandin D2 receptor 2-CRTH2) than for DP1. The G protein-coupled receptor for PGD2 is called CRTH2. When taken orally in multiple doses, setipiprant was well tolerated and in allergic asthmatics it decreased the allergen-induced lung inflammation as well as the related airway hyperresponsiveness. Treating allergic disorders may benefit from targeting CRTH2.
Targets |
hCRTH2 ( IC50 = 6 nM ); hDP1 ( IC50 = 1290 nM ); EP2 ( IC50 = 2600 nM )
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ln Vitro |
Setipiprant (0-10 μM; 90 min) interacts with the hCRTH2 receptor in the assay buffer both with and without human serum albumin (HSA) with IC50 values of 6 and 340 nM, respectively[1].
Setipiprant (0-10 μM; 5-20 min) inhibits human eosinophil shape change, intracellular cAMP release mediated by the hCRTH2 receptor, and IC50 values of 30, 80, and 235 nM, respectively[1]. Setipiprant (0-10 μM) inhibits the prostanoid receptors hDP1, hEP2, and hEP4 with IC50 values of 1290, 2600, and <10000 nM, respectively[1]. |
ln Vivo |
1.19 Pharmacokinetic properties of Setipiprant in rats and dogs [1]. AUC0-last (ng·h/mL) CL (mL/min/kg) T1/2 (hr) F (%) Rat IV 2 mg/kg 58500 1.3 6 44 Dog PO 10 mg/kg 91100 55
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References |
Molecular Formula |
C24H19FN2O3
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Molecular Weight |
402.41767
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Exact Mass |
402.14
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Elemental Analysis |
C, 71.63; H, 4.76; F, 4.72; N, 6.96; O, 11.93
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CAS # |
866460-33-5
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Appearance |
Solid powder
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SMILES |
C1CN(CC2=C1N(C3=C2C=C(C=C3)F)CC(=O)O)C(=O)C4=CC=CC5=CC=CC=C54
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InChi Key |
IHAXLPDVOWLUOS-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C24H19FN2O3/c25-16-8-9-21-19(12-16)20-13-26(11-10-22(20)27(21)14-23(28)29)24(30)18-7-3-5-15-4-1-2-6-17(15)18/h1-9,12H,10-11,13-14H2,(H,28,29)
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Chemical Name |
2-[8-fluoro-2-(naphthalene-1-carbonyl)-3,4-dihydro-1H-pyrido[4,3-b]indol-5-yl]acetic acid
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Synonyms |
Setipiprant; ACT-129968; ACT 129968; ACT129968; KYTH-105; KYTH105; KYTH 105
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~80 mg/mL (~198.8 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4850 mL | 12.4248 mL | 24.8497 mL | |
5 mM | 0.4970 mL | 2.4850 mL | 4.9699 mL | |
10 mM | 0.2485 mL | 1.2425 mL | 2.4850 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT02781311 | Completed | Drug: Setipiprant Drug: Placebo |
Alopecia | Allergan | July 14, 2016 | Phase 2 |
NCT01225315 | Completed | Drug: Setipiprant Drug: Placebo |
Asthma | Idorsia Pharmaceuticals Ltd. | November 1, 2010 | Phase 2 |
NCT02381496 | Completed | Drug: Setipiprant 500 mg Drug: Placebo |
Healthy | Idorsia Pharmaceuticals Ltd. | December 2011 | Phase 1 |
NCT01241214 | Completed | Drug: ACT-129968 Drug: Cetirizine |
Seasonal Allergic Rhinitis | Idorsia Pharmaceuticals Ltd. | November 2010 | Phase 2 |
NCT01877629 | Completed | Drug: ACT-129968 500 mg tablet Drug: ACT-129968 250 mg capsule |
Healthy Subjects | Idorsia Pharmaceuticals Ltd. | July 1, 2011 | Phase 1 |